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Functional Selectivity of G Protein-Coupled Receptor Ligands pp 267–281Cite as

Functional Selectivity at Non-Opioid Peptide Receptors

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Part of the book series: The Receptors ((REC))

Abstract

Pleiotropic signaling pathways activated by peptide hormone G protein-coupled receptors (GPCRs) are thought to mediate the physiological and pathogenic actions of these hormones. The mechanism by which the same ligand–receptor system mediates multiple effects is unclear. In general, cell-based discrepancy in signaling is thought to be responsible and accordingly drug development efforts have been refocused on modulating molecules downstream of receptors. Recent developments suggest that ligand–receptor systems are binary interaction units. A change in receptor or ligand will result in a specific change in functional outcome such as selective activation of pathways or skipping certain steps of a pathway. This phenomenon of ligand-induced functional selectivity is a new paradigm that could potentially lead to design of “smart” drugs that can enhance therapeutic potential of receptors and minimize potential adverse effects.

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Acknowledgments

Supported by NRSA grant # F32 HL088893 to Anushree Bhatnagar and RO1 grant # HL57470 to Sadashiva Karnik

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Authors and Affiliations

  1. Department of Molecular Cardiology, NB50 Lerner Research Institute, Cleveland Clinic Foundation, Cleveland, OH, 44195

    Sadashiva Karnik

Authors
  1. Anushree Bhatnagar
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  2. Sadashiva Karnik
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Corresponding author

Correspondence to Sadashiva Karnik .

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Editors and Affiliations

  1. VA Medical Center, 3710 SW US Veterans Hospital Road, 97239-2999, Portland, OR, USA

    Kim A. Neve

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© 2009 Humana Press, a part of Springer Science+Business Media, LLC

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Bhatnagar, A., Karnik, S. (2009). Functional Selectivity at Non-Opioid Peptide Receptors. In: Neve, K.A. (eds) Functional Selectivity of G Protein-Coupled Receptor Ligands. The Receptors. Humana Press. https://doi.org/10.1007/978-1-60327-335-0_13

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